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AR-A014418

(CAS No:487021-52-3)
AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM in cell-free assays, without significant inhibition on 26 other kinases tested.
CAS No:487021-52-3
Molecular Weight(MW):308.31
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 487021-52-3
Molecular formula(MF) C12H12N4O4S
Molecular Weight(MW): 308.31
Alias GSK-3β Inhibitor VIII;N-[(4-Methoxyphenyl)methyl]-N'-(5-nitro-2-thiazolyl)urea;N-[(4-Methoxyphenyl)Methyl]-N'-(5-nitro-thiazol-2-yl)urea
Solubility
In vitro DMSO 62 mg/mL (201.09 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
Biological Activity
Description AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM in cell-free assays, without significant inhibition on 26 other kinases tested.
Features Cell-permeable GSK3-selective inhibitor.
Targets
GSK-3β [1]
(Cell-free assay)
GSK-3β [1]
(Cell-free assay)
38 nM(Ki) 38 nM(Ki)
In vitro

AR-A014418 inhibits tau phosphorylation at a GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human four-repeat tau protein with IC50 of 2.7 μM, and protects cultured N2A cells from death induced by blocking PI3K/PKB pathway. In hippocampal slices, AR-A014418 inhibits neurodegeneration mediated by beta-amyloid peptide. [1] While in NGP and SH-5Y-SY cells, AR-A014418 reduces neuroendocrine markers and suppresses neuroblastoma cell growth. [2]

In vivo In ALS mouse model with the G93A mutant human SOD1, AR-A014418 (0-4 mg/kg, i.p.) delays the onset of symptoms, improves motor activity, slows down disease progression, and postpons the endpoint of the disease. [3] In addition, AR-A014418 produces inhibition effect on acetic acid- and formalin-induced nociception in mice by modulating NMDA and metabotropic receptor signaling as well as TNF-α and IL-1β transmission in the spinal cord. [4]